Synthesis of 7-thiaprostaglandin E1 congeners: Potent inhibitors of platelet aggregation.

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Abstract
Novel 7-thiaprostaglandin E1 derivatives and congeners were synthesized by a stepwise 3-component coupling process,which involves the introduction of .alpha.-side chains (thiols) and .beta.-side chains (organocopper reagents) into (R)-4-tert-butyldimethylsilyloxy-2-cyclopentenone. Several acid derivatives of 7-thiaprostaglandin E1 were also prepared either by enzymatic or by chemical methods. The stereochemistry of these products was assigned n the basis of the results with chiral protected cyclopentenones and chiral .omega.-side chains. Some of these 7-thiaprostaglandin E1 congeners exhibited more potent platelet aggregation-inhibitory actiity than PGE1. The structure-activity relationshp of these congeners is discused.

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